DOV-216,303 (Free Base) 是有效的5-羟色胺、去甲肾上腺素、多巴胺再摄取的三重抑制剂，其对 hSERT、hNET 和 hDAT 的IC50值分别为 14 nM，20 nM和78 nM。在嗅球切除大鼠模型中，可增加前额皮质中单胺的释放及具有抗抑郁的作用。
| 生物活性 | DOV-216,303 (Free Base) is a potent tripleserotonin,norepinephrine, anddopamine reuptakeinhibitor, withIC50values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively[1]. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats[2]. |
| IC50& Target | IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine)[1]. |
体内研究
(In Vivo) | Acute treatment of DOV-216,303 (20 mg/kg, i.p.) significantly increases dopamine, norepinephrine and serotonin levels in both OBX and Sham animals[2].
Chronic treatment with DOV 216,303 (20 mg/kg, i.p., for 17 days) increases extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increases extracellular baseline serotonin concentrations[2].
| Animal Model: | Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery[2]. | | Dosage: | 20 mg/kg. | | Administration: | I.P. daily for 17days. | | Result: | Increased extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increased extracellular baseline serotonin concentrations. |
| Animal Model: | Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery[2]. | | Dosage: | 20 mg/kg. | | Administration: | I.P. once. | | Result: | Significant increases in dopamine, norepinephrine and serotonin levels were measured in both OBX and Sham animals. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 125 mg/mL(547.96 mM) Ethanol : 100 mg/mL(438.37 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.3837 mL | 21.9183 mL | 43.8366 mL | | 5 mM | 0.8767 mL | 4.3837 mL | 8.7673 mL | | 10 mM | 0.4384 mL | 2.1918 mL | 4.3837 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (9.12 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.12 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (9.12 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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